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鉴定迷迭香酸为美国山茱萸的主要活性成分。

Identification of rosmarinic acid as the major active constituent in Cordia americana.

机构信息

Department of Pharmaceutical/Medicinal Chemistry, University of Tübingen, Germany.

出版信息

J Ethnopharmacol. 2010 Apr 21;128(3):561-6. doi: 10.1016/j.jep.2010.01.062. Epub 2010 Feb 10.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Preparation from leaves of Cordia americana have been widely used in traditional medicine in South Brazil to treat wounds and various inflammations.

AIM OF THE STUDY

The objective of this work was to identify the effective compounds in the ethanolic extract prepared from the leaves of Cordia americana, which is used in traditional South Brazilian medicine as anti-inflammatory and wound healing remedy.

MATERIALS AND METHODS

Isolation and structure elucidation techniques were performed in order to identify the compounds of Cordia americana and HPLC analysis was used for the quantification. The major constituent and the ethanolic extract were investigated for inhibition of 5-lipoxygenase, p38alpha MAPK, TNFalpha release and NF-kappaB as well as in the fibroblast scratch assay.

RESULTS

Rosmarinic acid (1) was identified as the major compound with an amount of 8.44% in the ethanolic extract of the leaves of Cordia americana. The ethanolic extract as well as (1) exhibited the highest inhibitory effects on 5-lipoxygenase (IC(50)=0.69 and 0.97microg/mL, resp., IC50 of BWA4C as reference: 0.3microM) and p38alpha (IC50=3.25 and 1.16microg/mL, resp., IC50 of SB203580 as reference: 0.046microM) and moderate inhibitory effects on TNFalpha release. Slight effects were observed in the fibroblast scratch assay.

CONCLUSIONS

This study increases our knowledge on the effective compound in Cordia americana and supports its use in traditional medicine. We demonstrated for the first time pharmacological effects of Cordia americana and we provide evidences for a crucial role of rosmarinic acid as the major key player.

摘要

民族药理学相关性

南美的 Cordia americana 的叶子制剂在南美的传统医学中被广泛用于治疗伤口和各种炎症。

研究目的

本工作的目的是鉴定 Cordia americana 叶乙醇提取物中的有效化合物,该提取物在南美的传统医学中被用作抗炎和愈合伤口的药物。

材料和方法

采用分离和结构鉴定技术来鉴定 Cordia americana 的化合物,并使用 HPLC 分析进行定量。对主要成分和乙醇提取物进行了 5-脂氧合酶、p38αMAPK、TNFα释放和 NF-κB 的抑制作用以及成纤维细胞划痕试验的研究。

结果

鉴定出迷迭香酸(1)为主要化合物,在 Cordia americana 叶的乙醇提取物中含量为 8.44%。乙醇提取物和(1)对 5-脂氧合酶(IC50=0.69 和 0.97μg/mL,分别为 BWA4C 作为参考的 IC50:0.3μM)和 p38α(IC50=3.25 和 1.16μg/mL,分别为 SB203580 作为参考的 IC50:0.046μM)的抑制作用最强,对 TNFα 释放有中等抑制作用。在成纤维细胞划痕试验中观察到轻微的作用。

结论

本研究增加了我们对 Cordia americana 中有效化合物的认识,并支持其在传统医学中的应用。我们首次证明了 Cordia americana 的药理作用,并提供了迷迭香酸作为主要关键成分的证据。

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